ES2208131A1 - Orally administered dietetic, nutritional supplement or medicament composition, useful as hypolipemic agent, comprising mixture of pectin and/or guar powder with eicosapentaenoic and docosahexaenoic acids - Google Patents

Abstract

An orally administered mixture (I) comprises (in daily dose amounts): (a) 5-30 g pectin and/or guar powder; and (b) 1-3 g of the (omega-3)-fatty acids EPA (eicosapentaenoic acid) and DHA (docosahexaenoic acid), as powder or capsules or in fish oil.

Description

Method for the manufacture of a medicine blood lipid level reducer for administration oral.

The invention relates to the use of a reducer of blood lipid levels for compound oral administration by a mixture of powdered omega-3 fatty acids which contains omega-3 acid fatty acids eicosapentaenoic acid (AEP) as well as docosahexaenoic acid (ADH) and pectin and / or guar as active substances as well as possible additional substances such as antioxidant vitamins, amino acids and trace elements.

Heart and circulation problems are the  No. 1 cause of death in Europe and the US with approx. 40% of All deaths. High blood levels of LDL lipids (low density lipoproteins) and VLDL triglycerides (very low density lipoproteins) are considered as factors of risk for heart and circulatory diseases. In this case,  the relationship of the `` bad '' LDL to the `` good '' HDL (high density lipoproteins) should not exceed the factor of 4: 1. As a reference value, in the world of medicine contemplates a total cholesterol content less than 200 as `` healthy '', but at an advanced age a value of about 250

High blood lipid levels are subject to oxidation and then lead to deposits in the vessel walls (arteriosclerosis). An answer is discussed increased immune, to be measured in increased values of PrC (PrC = reactive protein C), as a trigger for formation of plates as well as NO level (NO = nitric oxide) decreased by this pathological metabolic situation of high lipid levels in Blood and its oxidation.

For the reduction of blood lipid levels  Statins or the so-called CSE inhibitors are used. These inhibit the enzyme for endogenous cholesterol synthesis in the liver. It should be taken into account as a side effect that not only cholesterol synthesis is inhibited but also other processes of synthesis in the liver, such as the synthesis of steroid hormones (sex hormones) which can lead to disorders of the power.

Cholesterol is an important component of all cell membranes, so without cholesterol there are no cells suitable for living

As a side effect, CSE inhibitors they can disturb cell membrane formation to that extent which can lead to rhabdamolysis (destruction of muscle) with the death that results from it. Patients notice this in the initial stage with clear muscle aches.

The activity of the chemical inhibitor CSE / statin it is not often enough to reach the reference value alleged. Higher dosages or also combination therapies However, they increase the risk in terms of security.

If therapy with these failures considerably  substances, the doctor talks about a hyperlipemia of causes Genetic Just after the deaths of `` Lipobay '' has it is clear that more alternatives must be developed safe.

Fish oil (here it is contemplated as especially active the AEP) very well reduces the levels of triglycerides, in any case with the side effect of an increase of the LDL, of course most of the time, what after a few months ago it oscillates again to the pre-administration value of fish oil. ADH raises HDL levels.

High LDL values prior to Fish oil administration are also not reduced long term or only regularly and, therefore, insufficiently.

Pectin is a ballast substance and swelling (obtained from the pomace of apples and citrus fruits). one g of pectin absorbs up to 60 g of water, so that the pectin is predominantly used as a gelling agent. Hectic in liquid or yogurt / curd, pectin forms immediately large lumps that are swallowed with difficulty.

As ballast substances, both pectin and also save cholesterol in the intestine, predominantly in form of bile acids that contain cholesterol. It has been investigated the reduction of cholesterol levels by Ballast substances in hyperlipemias. The results, however, they were discreet so that they are not used in the world of medicine to reduce cholesterol level.

Since both ballast substances and also fish oil, respectively separately, have not shown no safe and sufficient reduction of the level of cholesterol, especially LDL, these substances are not Recommend or employ by doctors.

The task that serves as the basis for the invention is make available a blood lipid level reducer on which, in long-term employment in patients with hyperlipemia, can be administered in doses large enough to reduce meaningful way total cholesterol levels and those triglycerides without unwanted side effects neither short nor long term, especially those such as described with statins / CSE inhibitors.

In addition, a positive contribution of omega-3 fatty acids on stress blood, heart arrhythmias, myocardial infarction and risk of apopletic attack, atherosclerosis and about diseases inflammatory as reunite, psoriasis (psoriasis), osteoarthritis, colitis Ulcerative and Crohn's disease. Pectin and / or guar improve the evacuation in constipation and accelerate the passage through the intestine, so that toxic substances are excreted from the intestine more quickly

This task is solved by the reducer of blood lipid levels for oral administration according to the invention, which is characterized by a content of 1-3 g of omega-3 fatty acids (AEP and ADH) and 5-30 g of pectin and / or guar per dose daily

Surprisingly, the combined application of Omega-3 fatty acids with pectin or guar is a high-activity blood lipid level reducer, which not expected after the experience with the two groups of substances alone.

The Eskimos and Japanese do not have hyperlipemias due to its high consumption of fatty fish because it also contains many fatty acids at the same time omega-3 AEP and ADH. The native relationship in fish from AEP to ADH is, however, 2: 3, that is an AEP ratio to inverse ADH to what was used in the studies on oil fish.

In studies on fish oil, significantly reduced only the levels of triglycerides, but not LDL. In the mixture according to the invention, to the omega-3 fatty acid component of the blood lipid level reducer is given the relationship Native AEP: ADH of 2: 3.

More ADH forms more HDL, which carry the cholesterol from the body's cells to the liver.

With transport to the liver increased guarantees there an optimal formation of bile acids from cholesterol. Cholesterol delivered to the intestine through the Bile acids is bound there by pectin / guar before it can be resorbed from the intestine. In this case it is certain that the effectiveness of pectin / guar also depends on its quantity and the amount of available cholesterol.

ADH is necessary in the fetus and in newly born for brain formation (membranes and receptors) considering itself secured with sufficient contribution a better Maturation and intelligence.

The influence of ADH on the formation of recipients could also provide faster training of new receptors for the uptake of cholesterol from the cells of  the tissues. You just have to explain, then, that the Eskimos, that feed almost exclusively on seals, whales and fish fatty in ballast substances also presenting, so Therefore, saturated fats too much, do not have high levels of lipids in the blood.

AEP inhibits the release of fatty acids free of fatty tissue. AEP decreases enzymatic activity for the formation of triglycerides in the liver. Both actions lead to the reduction of triglyceride concentration in the blood. It also leads to enhanced conversion of rich VLDL in triglycerides in LDL that contain less triglycerides. In Correspondence can increase LDL cholesterol. A level of triglycerides well reduced is therefore a good guess for also successfully lower LDL.

The invention was tested in two people, men, middle-aged:

1. Since the CSE inhibitor (Lipobay) does not showed sufficient activity, the total cholesterol level was kept in the usual fluctuation interval, being diagnosed a hypercholesterolemia of genetic causes. After a month of administration of the AEP / ADH-pectin mixture According to the invention, the total cholesterol level was lowered from meaningful way.

       \ dotable {\ tabskip6pt # \ hfil \ + \ hfil # \ + \ hfil # \ + \ hfil # \ tabskip0ptplus1fil \ dddarstrut \ cr} {
 Year \ 1996 \ 1996 \1997 \ 1998 \ 1999
2000/2001 \ cr Total cholesterol \ quad \ + \ quad
350/317 \ 270 \ 270/316 \ quad \ + \ 392/255 \ cr
HDL \ + \ 40/39 \ quad \ + \ 42/50 \ quad \ +
61/64 \ cr LDL \ quad \ + \ quad 279/271 \ quad \ + \ quad
222/267 \ 26 \ 261/183 \ cr Triglycerides \ quad \ +
304/297 \ 224/346 \ quad \ + \ quad
349/196 \ cr LDL: HDL \ quad \ + \ quad 7: 1/7: 1 \ quad \ + \ quad
5.3: 1 / 5.3: 1 \ + \ quad
4.3: 1 / 2.8: 1 \ cr}
    

1996-1997 without medication (the fluctuation interval is in the usual frame), 1998-1999 with Lipobay (little action), 2000 without medication and as of 2001 with AEP / ADH-pectin (significant reduction of both triglyceride levels and also of the LDL). To prevent atherosclerosis due to risk factor of high blood lipid levels is favorable an LDL to HDL ratio of less than 4: 1.

2. Dialysis patient (than most sometimes you develop hyperlipemia) with a cholesterol level constant total of 300-320 without administration of medicines. After one month of administration of the mixture AEP / ADH-pectin according to the invention, the level of  Total cholesterol was reduced to 188 and in the following months remained at the lowest values. The ratio of LDL to HDL improved to 2: 1. At the same time the triglycerides of 415 were reduced to 225. The LDL did not increase due to the reduction of triglycerides but which were reduced simultaneously to 95.

       \ dotable {\ tabskip6pt # \ hfil \ + # \ hfil \ + # \ hfil \ tabskip0ptplus1fil \ dddarstrut \ cr} {
 Date 10.01.02 \ quad \ + \ quad 06.02.02 \ cr
Total Cholesterol \ 3 \ + \ 312 \ quad \ + \ 188 \ cr
HDL \ quad \ + \ quad 54 \ quad \ + \ quad 48 \ cr LDL \ quad \ +
Desc. 95 \ cr Triglycerides \ + \
415 \ + \ quad
225 \ cr}
    

For the state of knowledge of science current medical, completely unexpected and novel, the mixture according to the invention of pectin and fatty acids omega-3 with the active substances AEP and ADH in the 2: 3 native ratio (as in nature / in fish), reduces blood lipid levels in an order of magnitude that to date it was only known for chemical medications from CSE / statin inhibitor substance class.

The single reduction of lipid levels of the blood prevents, but not with enough security, a arteriosclerosis Fatty acids are subject to oxidation. Oxidized fat causes an inflammatory reaction that is discussed as the causal factor that triggers the formation of deposits.

Consequently, in another embodiment of the invention is recommended to enrich the mixture of AEP / ADH-pectin and / or guar with antioxidant vitamins C and E and / or the elements in traces, important for immune resistance, zinc and selenium (here there is an under-supply), as well as and / or the amino acid arginine that provides nitric oxide (NO). A sufficient level of nitric oxide in the blood is discussed in the sense that minimizes plaque adhesion to the arterial wall.

It is also appropriate to add to the mixture L-carnitine to ensure a penetration of lipids in tissue cells, since the L-carnitine acts as a carrier.

For diabetics it is appropriate to add also chrome together with the element in zinc traces, since in the both diabetic substances are excreted through the urine of augmented form but deal with a better tolerance to glucose.

A preferred embodiment according to the invention of the mixture of AEP / ADH-pectin and / or guar It is presented as follows:

Example 1 (portion daily)

5-15 g of pectin and / or guar and 1-3 g of AEP / ADH in the preferred ratio of 2 to 3, using omega-3 fatty acids in the form of powder or microcapsules stabilized against oxidation with vitamin C and / or E and adding, before mixing with pectin / guar, flavoring substances preferably with the smell of hazelnut-caramel, eventually some of vanilla.

Example 2 (portion daily)

Mix as example 1, but provided additionally with 200 mg of vitamin C, 100 mg of vitamin E.

Example 3 (portion daily)

Mix as example 2, but provided additionally with 15 mg of selenium and 15 mg of zinc and 200 µg of chrome.

Example 4 (portion daily)

Mix as example 3, but provided additionally with 5 g of arginine.

Claims (8)

1. Method for the manufacture of a blood lipid level reducing drug for oral administration, characterized in that 5-30 g of pectin and / or guar powder are mixed in a daily portion and

 \ hbox {1-3g} 

of omega-3 fatty acids AEP and ADH powder or microcapsules, also in the form of fish oil. 2. Method according to claim 1, characterized in that 50-1,000 mg of vitamin C and 25-500 mg ET (Tocopherol Equivalents) of vitamin E are additionally contained. 3. Method according to claim 1-2, characterized in that 10-60 mg of selenium and / or 5-30 mg of zinc and / or 100-200 µg of chromium are additionally contained. 4. Method according to claim 1-3, characterized in that 3-10 g of arginine are additionally contained. 5. Method according to claim 1-4, characterized in that all the active substances are contained in a powder, granulate or capsules or also parts thereof are included, e.g. ex. in the form of tablets, dragees or capsules, in a combined container. Method according to claim 1-5, characterized in that the ratio of omega-3 fatty acids from AEP to ADH corresponds to at least 2 to 3 to 2 to 5. 7. Method according to claim 1-6, characterized in that the omega-3 fatty acids AEP and ADH are in powder form or are microencapsulated and are protected against oxidation with the antioxidants vitamin C and vitamin E and / or rosemary, proceed of seaweed or fish oil and are protected from the smell and taste of fish with a flavoring, preferably with the smell of caramel hazelnut. Method according to claim 1-7, characterized in that it is a dietary food product, especially for medicinal purposes, a food supplement or a medicine, being packaged in portion bags, daily rations or larger containers such as, e.g. ex. boats